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DNA sequence-specific ligands. XVII. Synthesis, spectral properties, virological and biochemical studies of fluorescent dimeric bisbenzimidazoles DBA(n)

机译:DNA序列特异性配体。 十八。 荧光二聚体双质咪唑DBA(N)的合成,光谱特性,病毒学和生物化学研究

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摘要

A series of DNA minor groove binding fluorescent dimeric bisbenzimidazoles DBA(n) bearing linkers of various length were synthesized and their biochemical and antiviral activities were evaluated. Their antiviral activity was assessed in model cell systems infected with human herpes simplex virus (HSV-1) and cytomegalovirus (CMV). Compounds DBA(1) and DBA(7) demonstrated in vitro inhibitory properties towards HSV-1, and DBA(7) completely blocked the viral infection. Compound DBA(11) displayed the in vitro therapeutic activity towards both HSV-1 and CMV. All of the DBA(n) could fluoresce, were well soluble in water, not cytotoxic to a concentration of 240 mu M, penetrated well into cell nuclei by binding to DNA and could inhibit topo-I at low micromolecular concentrations. (C) 2018 Elsevier Ltd. All rights reserved.
机译:合成了一系列DNA小沟结合荧光二聚体双链咪唑DBA(N)轴承接头的DBA(N)轴承接头,并评估其生化和抗病毒活性。 在用人疱疹病毒(HSV-1)和巨细胞病毒(CMV)的模型细胞系统中评估了它们的抗病毒活性。 化合物DBA(1)和DBA(7)对HSV-1的体外抑制性能证明,DBA(7)完全阻止了病毒感染。 化合物DBA(11)向HSV-1和CMV展示了体外治疗活性。 所有DBA(n)都可以发荧光,在水中溶解,而不是细胞毒性至240μm的浓度,通过与DNA结合渗透到细胞核中,并且可以在低微分子浓度下抑制TOPO-1。 (c)2018年elestvier有限公司保留所有权利。

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    Russian Acad Sci Engelhardt Inst Mol Biol Vavilova St 32 Moscow 119991 Russia;

    Russian Acad Sci Engelhardt Inst Mol Biol Vavilova St 32 Moscow 119991 Russia;

    Russian Acad Sci Engelhardt Inst Mol Biol Vavilova St 32 Moscow 119991 Russia;

    Minist Hlth Russian Federat Ivanovsky Inst Virol Gamaleya Natl Res Ctr Epidemiol &

    Microbiol;

    Minist Hlth Russian Federat Ivanovsky Inst Virol Gamaleya Natl Res Ctr Epidemiol &

    Microbiol;

    Minist Hlth Russian Federat FSBI NN Blokhin Natl Med Res Ctr Oncol Inst Carcinogenesis;

    Minist Hlth Russian Federat FSBI NN Blokhin Natl Med Res Ctr Oncol Inst Carcinogenesis;

    Russian Acad Sci Engelhardt Inst Mol Biol Vavilova St 32 Moscow 119991 Russia;

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  • 正文语种 eng
  • 中图分类 药学;
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